کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1398112 1501206 2008 12 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis, biological evaluation and docking studies of 4-amino substituted 1H-pyrazolo[3,4-d]pyrimidines
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis, biological evaluation and docking studies of 4-amino substituted 1H-pyrazolo[3,4-d]pyrimidines
چکیده انگلیسی

The synthesis of new 4-amino substituted pyrazolo[3,4-d]pyrimidines along with their activity in cell-free enzymatic assays on Src and Abl tyrosine kinases is reported. Some compounds emerged as good dual inhibitors of the two enzymes, showed antiproliferative effects on two Bcr–Abl positive leukemia cell lines K-562 and KU-812, and induced apoptosis, as demonstrated by the PARP assay. Docking studies have been also performed to analyze the binding mode of compounds under study and to identify the structural determinants of their interaction with both Src and Abl.

A number of 4-amino substituted pyrazolo[3,4-d]pyrimidines have been synthesized and tested in cell-free enzymatic assays on Src and Abl tyrosine kinases. Some molecules emerged as good dual inhibitors and showed antiproliferative effects on leukemia cell lines, together with proapoptotic activity.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 43, Issue 12, December 2008, Pages 2665–2676
نویسندگان
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